5-Ht3 Receptor Antagonists

A kind of technology of CR5 and compound, applied in the field of 5-HT3 receptor antagonist

Active Publication Date: 2017-03-08
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 5-HT3 antagonists currently on the market are only approved for the treatment of vomiting or irritable bowel syndrome

Method used

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  • 5-Ht3 Receptor Antagonists
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  • 5-Ht3 Receptor Antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach (A

[0062] In one embodiment, the compound of formula (I) as defined in the Summary, or a pharmaceutical salt thereof, is wherein Z is O.

Embodiment approach (B

[0064] In one embodiment, the compound of formula (I) or a pharmaceutical salt thereof as defined in the Summary is wherein Z is NR a . Within this embodiment, in another group of compounds, R a is hydrogen. Within this embodiment, in another group of compounds, R a is methyl.

[0065] Implementation plan (C)

[0066] In another embodiment, a compound of formula (I) or a pharmaceutical salt thereof as defined in the general and above embodiments (A) and (B) and groups contained therein, in a group of compounds, R 1 is a ring with the formula

[0067]

[0068] (a) Within the group in embodiment (C), in a group of compounds, R 1 is a ring of formula (a) or (d). Within (a), in one embodiment, R 1 is a ring with the formula

[0069]

[0070] (b) Within the group of embodiments (C), in another group of compounds, R 1 is a ring of formula (e), (f) or (g). In (b), in a group of compounds, R 1 is a ring of formula (e). In (b), in a group of compounds, R 1 is a ring...

Embodiment approach (D

[0078] In another embodiment, in a group of compounds, a compound of formula (I) or a pharmaceutical salt thereof as defined in the summary and above in embodiments (A) and (B) and groups contained therein is wherein R 1 is a ring with the formula

[0079]

[0080] (a1) Within the group in embodiment (D), in a group of compounds, R 1 is a ring of formula (c) or (h). Within this embodiment, in a group of compounds, the stereochemistry at the chiral carbon is (R) or (S).

[0081] (b1) Within the group in embodiment (D), in a group of compounds, R 1 is a ring of formula (b).

[0082] (vi) In embodiment (D) and groups of embodiments contained therein (ie (a1) and (b1) and groups contained therein), in a group of compounds each R 3 are independently hydrogen or methyl. Within these groups of compounds, in a group of compounds, each R 3 is hydrogen.

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Abstract

The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Description

[0001] This application is a divisional application of the patent application with the application number 201380045326.X, the application date is July 16, 2013, and the invention name is "5-HT3 receptor antagonist". technical field [0002] The present invention provides compounds that are 5-HT3 receptor antagonists and are therefore useful in the treatment of diseases treatable by inhibition of 5-HT3 receptors, such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders and GI disorders. Also provided are pharmaceutical compositions containing the compounds and methods for preparing the compounds. Background technique [0003] The serotonin type 3 (5-HT3) receptor is part of the serotonergic system. Unlike the other receptors of this system, which are all G protein-coupled receptors, the 5-HT3 receptor is a ligand-gated ion channel and belongs to the superfamily of Cys-loop receptors, which Including nicotinic acetylcholine receptors, gamma-aminobuty...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/08C07D519/00A61K31/5386C07D221/22C07D451/12C07D453/02C07D471/04C07D471/08A61P25/04A61P29/00A61P25/30A61P25/28A61P25/00A61P25/18
CPCC07D221/22C07D451/12C07D453/02C07D471/04C07D471/08C07D498/08C07D519/00A61K31/19A61K31/5386A61P1/00A61P1/04A61P1/08A61P1/14A61P19/04A61P21/00A61P25/00A61P25/04A61P25/06A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P25/30A61P29/00A61P29/02A61P3/04A61P37/02A61P39/00A61P39/02A61P43/00A61P9/10C07D401/14C07D403/14C07D487/14C07D498/04C07C53/40C07C53/18
Inventor S·希驰库克H·蒙恩斯城H·雷查德孙会凯菊地正太T·麦克林M·霍普金斯
Owner TAKEDA PHARMA CO LTD
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